Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Douglas C. Knorr"'
Autor:
Nicholas Marcopulos, Gary M. Coppola, Beatriz Dardik, Paivi J. Kukkola, Jenny Tan, Hua Wang, Ricardo E. Chatelain, James L. Stanton, Alan D. Neubert, Natalie A. Bilci, Thomas D. Aicher, Arco Y. Jeng, Hollis C. Tomaselli, Douglas C. Knorr
Publikováno v:
Journal of Medicinal Chemistry. 48:6696-6712
High-throughput screening identified 5 as a weak inhibitor of 11beta-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some with low nanomolar inhibitory potency. A tertiary benzamide is required for biological activi
Autor:
Gary M. Coppola, Xilin Liu, Robert C. Anderson, Douglas C. Knorr, William S. Fillers, James L. Stanton, Jiaping Gao, Tomaselli Hc, Christine C. Vinluan, Thomas Daniel Aicher, Carol J. Dragland, Suraj S. Shetty, Wieslawa Maniara, A. Islam, Emma L. Kaplan, William R. Mann, Leonard J. Brand, Donald Mark Sperbeck, R. E. Walter, Dominick DelGrande, R. J. Lozito
Publikováno v:
Journal of Medicinal Chemistry. 43:236-249
N‘-Methyl-N-(4-tert-butyl-1,2,5,6-tetrahydropyridine)thiourea, SDZ048-619 (1), is a modest inhibitor (IC50 = 180 μM) of pyruvate dehydrogenase kinase (PDHK). In an optimization of the N-methylcarbothioamide moiety of 1, it was discovered that amid
Autor:
Emma L. Kaplan, Gary M. Coppola, Xilin Liu, Gregory Raymond Bebernitz, Donald Mark Sperbeck, Dominick DelGrande, Wieslawa Maniara, Leonard J. Brand, Suraj S. Shetty, Thomas Daniel Aicher, Robert C. Anderson, Charles F. Jewell, R. J. Lozito, Douglas C. Knorr, A. Islam, Chen Liu, Christine C. Vinluan, Jianping Gao, Robert J. Strohschein, William R. Mann, Carol J. Dragland, R. E. Walter
Publikováno v:
Journal of Medicinal Chemistry. 42:2741-2746
Autor:
Cheon Seung Hoon, Leonard J. Brand, Jeffrey Nadelson, Christina L. Leone, Rhonda O. Deems, Howard C. Smith, Douglas C. Knorr, Philip A. Bell, William S. Fillers, Thomas Daniel Aicher, Fell Jay Bradford, Ronald Simpson, Bork Balkan, Fraser James D, Gerald G. Kahle, Jiaping Gao
Publikováno v:
Journal of Medicinal Chemistry. 41:4556-4566
A series of substituted tetrahydropyrrolo[2,1-b]oxazol-5(6H)-ones and tetrahydropyrrolo[2,1-b]thiazol-5(6H)-ones was synthesized from amino alcohols or amino thiols and keto acids. A pharmacological model based on the results obtained with these comp
Publikováno v:
ChemInform. 30
In our investigations of potential hypoglycemic agents,2 it was desired to evaluate optically pure tetrahydropyrrolo[2,1-β]thiazol-5-ones. A novel, practical synthesis of each enantiomer of 1 via formation, separation, and hydrolysis of diastereomer
Autor:
Wei H. Wang, Christine C. Vinluan, Robert J. Strohschein, Xilin Liu, Emma L. Kaplan, Dominick DelGrande, Gregory Raymond Bebernitz, Douglas C. Knorr, Jennifer Tan, Jiaping Gao, Suraj S. Shetty, James L. Stanton, Charles Liu, Thomas Daniel Aicher, Carol J. Dragland, William R. Mann, Leonard J. Brand, Robert J. Lozito, Wieslawa Maniara, Amin Islam
Publikováno v:
Journal of medicinal chemistry. 43(11)
The optimization of a series of anilide derivatives of (R)-3,3, 3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase (PDHK) is described that started from N-phenyl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide 1
Autor:
Dario A. Otero, Philip A. Bell, Jeremy G. Dain, Thomas Daniel Aicher, Jeffrey Nadelson, Robert J. Strohschein, Leonard J. Brand, Douglas C. Knorr, James E. Foley, Douglas A. Young, Gregory Raymond Bebernitz, Ronald Simpson, William S. Fillers, Rhonda O. Deems
Publikováno v:
Journal of medicinal chemistry. 42(1)
SAH 51-641 (1) is a potent hypoglycemic agent, which acts by inhibiting hepatic gluconeogenesis. It is a prodrug of 4-(2, 2-dimethyl-1-oxopropyl)benzoic acid (2) and 4-(2, 2-dimethyl-1-hydroxypropyl)benzoic acid (3), which sequester coenzyme A (CoA)
Publikováno v:
Tetrahedron Letters. 39:8579-8580
In our investigations of potential hypoglycemic agents,2 it was desired to evaluate optically pure tetrahydropyrrolo[2,1-β]thiazol-5-ones. A novel, practical synthesis of each enantiomer of 1 via formation, separation, and hydrolysis of diastereomer
Autor:
Max Denzer, L. C. Iorio, R. J. Strohschein, G. Corriveau, Galantay Eugene E, R. Simpson, Ryan Ea, Douglas C. Knorr, N. A. Paodella, John H. Gogerty, Y. Uike
Publikováno v:
Chemischer Informationsdienst. 6